GW 4064

Cat. No. 2473

GW 4064 C28H22Cl3NO4 [278779-30-9]

Price and Availability

For GW 4064 pricing & availability please select your country from the drop down menu:
Submit
By clicking submit you agree to accept a cookie from Tocris Bioscience. For details, please read our privacy and cookie policy.

Chemical Name: 3-[2-[2-Chloro-4-[[3-(2,6-dichlorophenyl)-5-(1-methylethyl)-4-isoxazolyl]methoxy]phenyl]ethenyl]benzoic acid

Biological Activity

Selective, non-steroidal farnesoid X receptor (FXR) agonist (EC50 = 15 nM). Displays no activity at other nuclear receptors at concentrations up to 1 μM. Improves hyperglycaemia and hyperlipidemia in diabetic db/db mice. Shown to suppress autophagy in nutrient-deprived mouse hepatocytes.

Licensing Information

Sold for research purposes under agreement from GlaxoSmithKline

Technical Data

M.Wt:
542.84
Formula:
C28H22Cl3NO4
Solubility:
Soluble to 100 mM in DMSO and to 10 mM in ethanol
Purity:
>97 %
Storage:
Desiccate at +4°C
CAS No:
278779-30-9

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

Certificate of Analysis / Product Datasheet
Select another batch:

Lee et al (2014) Nutrient-sensing nuclear receptors coordinate autophagy. Nature 516 112. PMID: 25383539.

Cariou et al (2006) The farnesoid X receptor modulates adiposity and peripheral insulin sensitivity in mice. J.Biol.Chem. 281 11039. PMID: 16446356.

Zhang et al (2006) Activation of the nuclear receptor FXR improves hyperglycemia and hyperlipidemia in diabetic mice. Proc.Natl.Acad.Sci.USA 103 1006.

Maloney et al (2000) Identification of a chemical tool for the orphan nuclear receptor FXR. J.Med.Chem. 43 2971. PMID: 10956205.

If you know of a relevant reference for this product please let us know.

Citations are publications that use Tocris products. Selected citations for GW 4064 include:

Gomez-Ospina et al (2016) Mutations in the nuclear bile acid receptor FXR cause progressive familial intrahepatic cholestasis. J Hematol Oncol 7 10713. PMID: 26888176.

Hoeke et al (2014) Human FXR regulates SHP expression through direct binding to an LRH-1 binding site, independent of an IR-1 and LRH-1. PLoS One 9 e88011. PMID: 24498423.

Lee et al (2014) Nutrient-sensing nuclear receptors coordinate autophagy. Nature 516 112. PMID: 25383539.

Rondini et al (2014) Regulation of human cytosolic sulfotransferases 1C2 and 1C3 by nuclear signaling pathways in LS180 colorectal adenocarcinoma cells. J Clin Invest 42 361. PMID: 24335393.

Dai et al (2011) Impact of bile acids on the growth of human cholangiocarcinoma via FXR. Drug Metab Dispos 4 41. PMID: 21988803.

Fu et al (2011) Bile acid stimulates hepatocyte polarization through a cAMP-Epac-MEK-LKB1-AMPK pathway. Proc Natl Acad Sci U S A 108 1403. PMID: 21220320.

Fickert et al (2009) Farnesoid X receptor critically determines the fibrotic response in mice but is expressed to a low extent in human hepatic stellate cells and periductal myofibroblasts. Am J Pathol 175 2392. PMID: 19910507.

Do you know of a great paper that uses GW 4064 from Tocris? If so please let us know.show all ▼show less ▲

View Related Products by Target

View Related Products by Product Action

Keywords: GW 4064, supplier, Selective, farnesoid, X, receptor, FXR, agonists, Receptors, Liver, LXR-like, GW4064, GlaxoSmithKline, GSK, Tocris Bioscience, LXR-like Receptor Agonist products

Quick Order

Find multiple products by catalog number

divider line

Cancer Research Product Guide

Cancer Research Product Guide

Our Cancer Research Guide highlights over 750 products for cancer research. Request copy or view PDF today.

divider line

Nuclear Receptors Product Listing

Nuclear Receptors Product Listing

Our Nuclear Receptors Listing highlights over 150 products for nuclear receptors. Request copy or view PDF today.

divider line

New Products in this Area

EC 19

Synthetic retinoid; induces differentiation of stem cells

SI-2 hydrochloride

Steroid receptor coactivator 3 (SRC-3) inhibitor

SR 0987

T cell-specific RORγ (RORγt) agonist

WAY 252623

Potent LXR agonist

SR 9009

Rev-Erbα/β agonist

Sign-up for new product e-alerts
divider line

Twitter Updates

Follow @Tocris on Twitter

Follow us on Twitter!

Tocris is now actively tweeting. For regular updates on news, events and special offers, follow @Tocris on Twitter.